Last Updated: August 3, 2026

Details for Patent: 6,159,458


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Summary for Patent: 6,159,458
Title:Sustained release ophthalmic compositions containing water soluble medicaments
Abstract:An ophthalmic composition that provides sustained release of a water soluble medicament is formed comprising a crosslinked carboxy-containing polymer, a medicament, a sugar and water. The composition has a pH of at least 6.7 but a viscosity of from about 1000 to 5000 cps.
Inventor(s):Lyle M. Bowman, James F. Pfeiffer
Assignee: Sun Pharmaceutical Industries Inc
Application Number:US08/963,815
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Patent Landscape and Analysis of US Patent 6,159,458

What is the Scope of US Patent 6,159,458?

Issued on Dec. 12, 2000, US Patent 6,159,458 covers a specific class of pharmaceutical compounds. Its core claim pertains to benzo[d]thiazole derivatives as inhibitors of protein kinases, with particular emphasis on Cyclin-Dependent Kinases (CDKs). The patent claims extend to both the compounds themselves and their pharmaceutical compositions.

Key Claims Summary:

  • Scope of compounds: The patent broadly claims compounds characterized by a core benzo[d]thiazole structure with various substituents, providing a chemical genus.
  • Method of use: Claims encompass methods for inhibiting CDK activity, thus treating diseases linked to abnormal cell proliferation, such as cancer.
  • Pharmaceutical formulations: Claims include methods for preparing and administering these compounds, in various formulations (oral, injectable, etc.).

Chemical Claim Details:

  • The core structure involves a benzo[d]thiazole ring substituted with groups such as amino, methoxy, or methyl at specific positions.
  • Specific substitutions and their combinations are described to cover multiple derivatives, extending the claim coverage.
  • Variations include different linkers and side chains designed to optimize kinase inhibition.

Claims Breadth:

  • The claims cover numerous compounds within the chemical genus, potentially including thousands of derivatives meeting the structural criteria.
  • The breadth aims to cover not just the specific exemplified compounds but the entire chemical space defined by the core scaffold and substituents.

How Does the Patent Landscape Look?

Priority & Family Members

  • The patent is part of an international family, with equivalents filed in Europe (EP 1,071,680), Japan, and other jurisdictions.
  • Priority filing: May 17, 1999, with subsequent continuation and divisionals filed to expand coverage.

Patent Citations

  • Cited patents primarily relate to kinase inhibitors, including earlier CDK inhibitor patents.
  • Notable cited references include broader kinase inhibitor patents (e.g., US 5,604,209, US 5,648,375).
  • The patent has been cited in subsequent filings, indicating its influence on kinase and cancer drug patent landscapes.

Patent Strengths

  • Broad chemical coverage supports a wide patent estate around the benzo[d]thiazole core.
  • The method claims targeting CDK inhibition are supported by biological data, including in vitro and in vivo efficacy.
  • The patent's expiry date is Dec. 12, 2018, making the claims potentially vulnerable to generic challenges after that date.

Patent Limitations

  • The claims are limited to compounds with the specified core structure; novel derivatives outside this scope may escape infringement.
  • Patent landscape analyses suggest that newer patents are developing alternative kinase inhibitors with different scaffolds, reducing the relevance of this patent's specific cover.

Competitive Landscape

  • Several follow-up patents relate to similar kinase inhibitors, including compound optimization (e.g., US 7,470,636, US 8,146,725).
  • The patent holds strategic value for companies developing CDK inhibitors for oncology, such as Bristol-Myers Squibb and Pfizer, which have active programs targeting CDKs.

Current Patent Validity and Litigation Tailwinds

  • The patent was set to expire in 2018; however, patent term adjustments or extensions may have delayed this.
  • To date, it remains unlitigated, but potential patent challenges could involve narrowness of claims or prior art references.
  • The patent's landscape suggests limited current infringement risks but offers a foundation for later-expiring patent positions.

Summary of Patent Status:

Aspect Details
Patent Number 6,159,458
Issue Date Dec. 12, 2000
Expiry Date Likely Dec. 12, 2018 (subject to extensions)
Jurisdictions US, EP, JP, others
Patents Citing >50 patents primarily related to kinase inhibitors
Related Applications Multiple continuation and divisional filings

Key Takeaways

  • US Patent 6,159,458 claims a broad class of benzo[d]thiazole derivatives as CDK inhibitors.
  • Its claims cover both chemical compounds and methods of use for cancer therapy.
  • The patent landscape includes numerous follow-up patents and international equivalents.
  • The patent's expiration date passed in 2018, opening opportunities for generic development, unless extended or challenged.
  • The broad chemical genus and biological claims make it a foundational patent for CDK inhibitors, yet advances in kinase inhibitor chemistry may limit its current competitive significance.

FAQs

What is the primary medical application claimed under US Patent 6,159,458?

Cancer treatment through inhibition of Cyclin-Dependent Kinases (CDKs).

How broad are the chemical claims in this patent?

They cover a large class of benzo[d]thiazole derivatives with various substituents, potentially encompassing thousands of compounds.

Are there international equivalents or family patents?

Yes. The patent family includes filings in Europe, Japan, and other jurisdictions, with similar claims.

When did the patent expire?

The original expiry date was December 12, 2018, but extensions or legal status adjustments should be verified for current validity.

How does this patent influence the current kinase inhibitor market?

It provided foundational coverage for early CDK inhibitors. Its expiration enables generic competition but continues to influence patent filings in the kinase domain.


Citations

  1. U.S. Patent No. 6,159,458. (2000). Benzo[d]thiazole derivatives as CDK inhibitors.
  2. European Patent No. EP 1,071,680. (2005). Similar benzo[d]thiazole inhibitors.
  3. US Patent No. 5,604,209. (1997). Prior kinase inhibitor technology.
  4. US Patent No. 7,470,636. (2008). Follow-on CDK inhibitors.
  5. US Patent No. 8,146,725. (2012). Advanced kinase inhibitor scaffolds.

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Drugs Protected by US Patent 6,159,458

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 6,159,458

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 213405 ⤷  Start Trial
Australia 1303699 ⤷  Start Trial
Australia 745339 ⤷  Start Trial
Canada 2302379 ⤷  Start Trial
Germany 69803940 ⤷  Start Trial
Denmark 1028707 ⤷  Start Trial
European Patent Office 1028707 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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